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Quantitative relationship between rat intestinal absorption and Abraham descriptors.

机译:大鼠肠道吸收与亚伯拉罕描述子之间的定量关系。

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摘要

Literature data on the intestinal absorption of 158 drug and drug-like compounds in rats have been collected, and Abraham descriptors for the set of drugs have been calculated using the method of Platts and Abraham et al. Results show that there is a significant relationship between rat intestinal absorption and the Abraham descriptors. In agreement with the human intestinal absorption model, the dominant descriptors in the rat model are the drug hydrogen bond acidity and basicity. In order to compare the absorption models in humans and rats, the absorption model developed from rats was used to predict the absorption in humans. The rat intestinal absorption model is similar to the human absorption model, and data on rats can effectively be used to predict human intestinal absorption.
机译:收集了关于大鼠中158种药物和类药物化合物的肠道吸收的文献资料,并使用Platts和Abraham等人的方法计算了这组药物的亚伯拉罕描述词。结果表明,大鼠肠道吸收与亚伯拉罕描述子之间存在显着关系。与人类肠道吸收模型一致,大鼠模型中的主要描述词是药物氢键的酸度和碱性。为了比较人和大鼠的吸收模型,使用从大鼠建立的吸收模型来预测人的吸收。大鼠肠道吸收模型与人体吸收模型相似,并且大鼠数据可有效地用于预测人体肠道吸收。

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